Is it easy to stop RNA polymerase?

Artsimovitch I; Vassylyev DG

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Is it easy to stop RNA polymerase?

机译：停止RNA聚合酶容易吗？

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Among transcription factors that bind to bacterial RNA polymerase (RNAP) and modulate its activity, a number of small molecules irreversibly inhibit RNAP thereby causing cell death. To be of clinical significance such inhibitors must (1) inhibit a broad range of bacterial RNAPs but not affect human cells, (2) penetrate bacterial cell walls and (3) circumvent bacterial resistance mechanisms. Rifamycins, the only class of RNAP inhibitors that have found their way into clinical practice, are widely used in the treatment of tuberculosis and leprosy. However, the practical value of this class of antibiotics is limited by a rapid rise in resistant bacterial isolates. In this review we focus on recent advances in studies of prokaryotic transcription that allow a detailed structural and functional characterization of a number of RNAP/rifamycins complexes, thereby opening new opportunities for the design of superior antibacterial agents.

机译：在与细菌RNA聚合酶（RNAP）结合并调节其活性的转录因子中，许多小分子不可逆地抑制RNAP，从而导致细胞死亡。为了具有临床意义，此类抑制剂必须（1）抑制多种细菌RNAP，但不影响人类细胞;（2）穿透细菌细胞壁;（3）规避细菌抗性机制。利福霉素是已进入临床实践的唯一一类RNAP抑制剂，已广泛用于治疗肺结核和麻风病。但是，这类抗生素的实用价值受到耐药菌分离物的迅速增加的限制。在这篇综述中，我们着重于原核转录研究的最新进展，这些进展允许对许多RNAP /利福霉素复合物进行详细的结构和功能表征，从而为设计卓越的抗菌剂提供了新的机会。

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《Cell cycle》 |2006年第4期|共6页
作者
Artsimovitch I; Vassylyev DG;
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正文语种 eng
中图分类细胞生物学;
关键词
Anti-Bacterial Agents; DNA-Directed RNA Polymerases;

机译：抗细菌剂;DNA定向RNA聚合酶;

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Is it easy to stop RNA polymerase?

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